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RN486

更新时间:2024-01-16 18:16:44

常用名 RN486 CAS号 1242156-23-5
价格 ¥需询单/1kg ¥需询单/1g ¥需询单/1mg 纯度 98.0%
备货期 需询单 库存 询单
 产品详情(用途,包装等)
用途:
RN486 is a selective Btk inhibitor with an IC50 Value of 4.0 nM.IC50 Value: 4.0 nM [1]Target: Btk Kinasein vitro: In the enzymatic assay, the compound potently inhibited Btk kinase activity with an IC50 of 4.0 nM. RN486 not only potently and selectively inhibited the Btk enzyme, but also displayed functional activities in human cell-based assays in multiple cell types, blocking Fcε receptor cross-linking-induced degranulation in mast cells (IC(50) = 2.9 nM), Fcγ receptor engagement-mediated tumor necrosis factor α production in monocytes (IC(50) = 7.0 nM), and B cell antigen receptor-induced expression of an activation marker, CD69, in B cells in whole blood (IC(50) = 21.0 nM) [1]. In a co-culture system consisting of human primary synovial FLS and activated human platelets, convulxin stimulation resulted in elevated production of pro-inflammatory cytokines, IL-6 and IL-8, an effect which was dose-dependently blocked by RN486 [2].in vivo: RN486 displayed similar functional activities in rodent models, effectively preventing type I and type III hypersensitivity responses. More importantly, RN486 produced robust anti-inflammatory and bone-protective effects in mouse CIA and rat adjuvant-induced arthritis (AIA) models. In the AIA model, RN486 inhibited both joint and systemic inflammation either alone or in combination with methotrexate, reducing both paw swelling and inflammatory markers in the blood [1]. The administration of RN486 completely stopped disease progression, as determined by histologic and functional analyses of glomerular nephritis. The efficacy was associated with striking inhibition of B cell activation, as demonstrated by a significant reduction in CD69 expression in response to BCR crosslinking. RN486 markedly reduced the secretion of IgG anti-double-stranded DNA (anti-dsDNA) secretion, as determined by enzyme-linked immunosorbent and enzyme-linked immunospot assays [3].
物理化学性质:
CAS号:1242156-23-5
常用中文名:RN486
常用英文名:RN486
分子式:C35H35FN6O3
分子量:606.689
密度:1.4±0.1 g/cm3
沸点:868.6±65.0 °C at 760 mmHg
熔点:N/A
闪点:479.1±34.3 °C
储存条件:-20℃

供应商信息

上海楼岚生物科技有限公司

认证状态:未认证供应商
电话:52996696
地址:沪南路2729弄1310号
地区: 上海市 上海市 浦东新区
联系人:孙先生
联系人电话:021-52996696
邮件:sales@lollanechem.com
网址:http://www.bioll.com
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参考价格:$208/10mM*1mLinDMSO
其他供应商价格:
2024-03-12 RN486
价格:¥6488.9
2020-12-08 RN486
价格:¥需询单

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